Aim To study the effect of novel AChE inhibitors, 2-phenoxy-indan-1-one derivatives (YKY-1~7), against glutamatic acid-induced neurotoxicity in PC12 cells and on learning & memory impairment in dementia model mice induced by A?25~35 icv Methods The PC12 cells were preincubated with different concentrations of YKY-1~7 for 24 h and subsequently treated by glutamatic acid, at the high concentration of 2 mmol?L-1 for 15 min to induce cytotoxicity. The cell viability was assessed with MTT method.. Dementia model mice were made by intracerebroventricular injection (icv) of aggregated A?25~35. From the next day, the model mice were administered YKY-7 (2.5, 5, 10 mg?kg-1, ig) for 10 consecutive days and sham control mice or A? model control mice received daily ig saline. After the final treatment, the passive avoidance learning was tested, regional cerebral blood flow at cerebral cortex was assessed, and the activity of AChE in the cerebral cortex, hippocampus and blood serum were determined. Results Six out of the seven YKY compounds appeared to be effective against glutamatic acid-induced neurotoxicity in PC12 cells, with YKY-7 demonstrating the most activity. YKY-7 significantly ameliorated the learning and memory ability in dementia model mice induced by A?25-35 icv, slightly and selectively inhibited the cortical and hippocampal AChE, and gently increased the blood flow at cerebral cortex. Conclusion Some of 2-phenoxy-indan-1-one derivatives reported here have protective effects against glutamatic acid induced neurotoxicity in PC12 cells, and improve the learning and memory impairment induced by A?25-35, which may be partly attributable to its selective inhibition of AChE activity in the cerebral cortex and hippocampus.

Adolescent ; Child ; Humans ; Male ; Manipulation, Orthopedic ; methods ; Radius Fractures ; therapy

Volatile oil components and the contents and types of amino acid in spica of Prunella vulgaris were analysed by GC-MS and amino acid analyzer. Esters, fatty acids, aromatic hydrocarbon, ketone and several alcohol compounds were identified by mass spectrum comparison. In these ingredients, beta-ionone smelled aroma of cedar, raspberry, nerolidol showed weak sweet soft orange blossom flavor, neroli tasted sweet and fresh, nerolidol tasted sweet with light aroma of wood, hexadecanal showed a weak aroma of flowers and wax, alpha-sinensal had rich and fresh sweet orange flavor. To some extent, these types of aromatic substances can affect the taste of herbal tea or decoction made of Spica Prunellae. Among amino acids detected, natural amino acids accounted for a larger proportion, and those natural amino acids showed bitterness, slight bitterness, sourness (freshness), sweetness, slight sweetness, sourness (slight freshness). The results indicated that bitter and slightly bitter amino acids have the greatest impacts on the sense of Spica Prunellae.
Amino Acids ; analysis ; Gas Chromatography-Mass Spectrometry ; Oils, Volatile ; analysis ; Prunella ; chemistry ; Taste

Objective To investigate the correlation ofClaudin-1, Ki-67 and CD34 expressionsin the tumor tissue to the invasiveness, grading and proliferation of astrocytic tumors. Methods In 50cases of astrocytic tumor, the expressions of Claudin-1, IO-67 and CD34 were detectedimmunohistochemically in the tumor tissue, normal brain tissues and in the junctional area between thetumor and normal tissues. The expressions of Claudin-1, Ki-67, and CD34 were analyzed in relation tothe clinicopathoiogical characteristics of the patients. Results The expression rate of Claudin-1 was70.59% in the astrocytic tumors of histological grades Ⅰ and Ⅱ, significantly higher than that in grade Ⅲand Ⅳ tumors (9.09%, χ2=20.206, P=0.000). In grade Ⅲ and Ⅳ tumors, the positivity rates of Ki-67 inthe normal tissues, junctional area and the tumor tissue were all significantly higher those in grade Ⅲ andⅣ tumors (t=9.144, 5.958, and 6.297; P=0.000, 0.000, and 0.000, respectively). Grade Ⅲ and Ⅳ tumorsdisplayed significantly greater mierovessel density (MVD) than grade Ⅰ and Ⅱ tumors in the tumor tissue(t=3.101, P=0.003) and the junctional area (t=4.139, P=0.000). In all the tumors, significantly higherKi-67 expression was seen in the tumor tissue (12.74±6.93) than in the junctional area (7.42±3.93) andthe normal tissue (3.22±1.57) (F=51.726, P=0.000), and the MVD was also greater in the tumor tissue(27.48±8.26) than in the junctional area (10.72±3.93) and normal tissue (6.48±1.45) (F=215.538, P=0.000).Conclusion Expressions of Claudin-1, Ki-67, and CD34 are closely correlated to the proliferation andinvasion of astrocytic tumors, and these cytokines may serve as important indicators for evaluating themalignancy of astrocytic tumors..

OBJECTIVE: To develop a method to measure trihexyphenidyl, chlorpromazine and clozapine in human blood with GC-MS. METHODS: The specimens were alkalized (pH > 10) and extracted with V (benzene):V(ethyl acetate) = 1:1, and qualitatively analyzed using GC-MS-Full Scan with internal standard SKF525A. The specimens were alkalized (pH > 10) and extracted with V(benzene):V(ethyl acetate) = 1:1, and quantitatively analyzed using GC-MS-SIM with internal standard diazepam-d5. RESULTS: The lowest detection limits of trihexyphenidyl, chlorpromazine and clozapine were 0.3, 0.3 and 0.7 ng/mL (S/N > or = 3) respectively. The calibration curve in 20-10 000 ng/mL showed a good linear distribution. The recovery rate was 79.9% to 85.5%. The RSDs of intraday and interday were less than 5.1%. CONCLUSION The established method was simple, sensitive and accurate for simultaneous determination of trihexyphenidyl, chlorpromazine and clozapine in human blood, and can be applied in forensic toxicological cases.
Adult ; Antipsychotic Agents/poisoning* ; Chlorpromazine/blood* ; Clozapine/blood* ; Female ; Forensic Toxicology ; Gas Chromatography-Mass Spectrometry/methods* ; Humans ; Hydrogen-Ion Concentration ; Male ; Middle Aged ; Reproducibility of Results ; Sensitivity and Specificity ; Solvents/chemistry* ; Trihexyphenidyl/blood*

OBJECTIVETo investigate the impact of early rapid virological response on the outcomes of hepatitis B associated acute on chronic liver failure during antiviral treatment.

METHODS106 acute on chronic liver failure patients in our hospital from January 2008 to July 2010 were enrolled in present study retrospectively. Besides internal medicine therapy, all patients received lamivudine (100 mg/d) or entecavir (0.5 mg/d) treatment. The profile of liver biochemistry, prothrombin time activity and viral load were detected at baseline and week 4, respectively. The patients were divided into HBV DNA negative group and HBV DNA positive group according to the viral load at week 4. The clinical features and treatment outcomes were compared between groups. Frequency variables were compared by x2 test or Fisher's exact test. Continuous variables were compared using independent samples T-test. The factors that impact on the treatment outcomes were determined using stepwise multivariate logistic regression analysis.

RESULTSAt the week 4, the TBil and PTA in HBV DNA positive group [(261.6+/-205.6)mumol/L and 44.7%+/-19.7%, respectively] were significantly different from those in HBV DNA negative group [(160.1+/-173.4) mumol/L and 56.8%+/-23.1%, respectively] ( t = 2.190 and -2.077, respectively, P less than 0.05). The non-effective rate of HBVDNA positive group (50%, 9/18) was significantly higher than that of HBV DNA negative group (14.8%, 13/88) (x2 = 9.235, P less than 0.01). By using stepwise multivariate logistic regression analysis, the disease stage and HBV DNA undetectable at week 4 were the independent factor. The OR values of disease stage and HBV DNA undetectable were 6.559 and 0.209, respectively, and 95% CI was 2.316~18.576 and 0.058~0.747, respectively.

CONCLUSIONThe rapid suppression of viral load by nucleotide analogue may improve the efficacy of hepatitis B associated acute on chronic liver failure treatment. The early rapid virological response within first 4 weeks may contribute to the prediction of the treatment outcomes.

Adult ; Antiviral Agents ; therapeutic use ; DNA, Viral ; blood ; End Stage Liver Disease ; drug therapy ; virology ; Female ; Hepatitis B ; drug therapy ; Humans ; Liver Failure, Acute ; drug therapy ; virology ; Male ; Middle Aged ; Prognosis ; Retrospective Studies ; Treatment Outcome ; Viral Load

OBJECTIVETo discuss the feasibility and safety of different approaches for CT-guided percutaneous needle biopsy and subsequent iodine-125 seed interstitial implantation for pancreatic cancer.

METHODSA retrospective study was carried out on the complete data of 35 patients with pancreatic cancer who have received CT-guided percutaneous needle biopsy with or without subsequent iodine-125 seed interstitial implantation. There were 9 lesions located in the head of pancreas, 20 located in the body, and 6 in the tail. The maximum diameter of the lesions varied from 12 mm to 60 mm (mean 37.1 mm). The patients were treated with a needle in diameter of 16-21G. Operations were undertaken via anterior, posterior and lateral approaches.

RESULTSThirty-five patients underwent 43 times of CT-guided percutaneous needle biopsies. Thirty-one cases were pathologically diagnosed as cancer, 2 cases inflammatory lesions, and 2 were suspected tumors (one of which was finally diagnosed as cancer, while another was pancreatic pseudocyst). The ratio of correct diagnosis was 94.3%. Fourteen patients were treated subsequently with CT-guided iodine-125 seed interstitial implantation therapy, with a total of 65 times of needle puncture. The operations were performed via direct approach to the tumor in 18 cases, transhepatic approach in 2 cases, transgastric approach in 4 cases, transintestinal approach in 10 cases, and through mesenteric vessels in one case. Incidence of complications in the biopsy group was 2.32% (1/43), and in the implantation group was 6.15% (4/65), with a statistically non-significant difference (P = 0.600) between the two groups. Incidence of complications in the group using 16-18G needle was 4.65% (4/86), while in the group using 20-21G needle was 4.55% (1/22), also with a non-significant difference (P = 0.064). The accuracy rate of needle biopsy in this study was 94.28% (33/35).

CONCLUSIONCT-guided percutaneous needle biopsy and subsequent iodine-125 seed interstitial implantation are both feasible and safe for pancreatic cancer.

Adult ; Aged ; Aged, 80 and over ; Biopsy, Needle ; methods ; Brachytherapy ; methods ; Female ; Follow-Up Studies ; Humans ; Iodine Radioisotopes ; therapeutic use ; Male ; Middle Aged ; Pancreatic Neoplasms ; diagnostic imaging ; pathology ; radiotherapy ; Radiography, Interventional ; methods ; Retrospective Studies ; Tomography, X-Ray Computed

OBJECTIVETo investigate the effects of peritoneal dialysis solution (PDS) on apoptosis and intracellular free calcium([Ca(2+)]i), cell surface ICAM-1 expression of rat peritoneal mesothelial cells (RPMCs).

METHODSThe RPMCs apoptosis rate were determined by flow cytometry. [Ca(2+)]i in the cells were monitered the fluorescence at 528 nm by confocus laser microscopy. Cell surface ICAM-1 expression were detected by flow cytometry.

RESULTAfter PDS treatment for 1 h, the RPMCs apoptosis rate were increased. Such increase was more manifest with higher glucose concentration in PDS and longer treatment time of the cells. At the same times, after 3 hours, ICAM-1 expressions of the PDS containing glucose and mannitol are all increased. With the increase of glucose concentrations, the descend of [Ca(2+)]i levels were aggravated.

CONCLUSIONPDS containing high- concentration glucose can induce significant apoptosis of RPMCs in vitro. This may be related with the enhanced level of ICAM-1 expressions and the decreased level of [Ca(2+)]i. Which may due to the occurrence of peritoneal fibrosis and ultrafiltrate failure in patients suffering long term peritoneal dialysis.

Animals ; Apoptosis ; drug effects ; Calcium ; metabolism ; Dialysis Solutions ; pharmacology ; Dose-Response Relationship, Drug ; Epithelial Cells ; cytology ; drug effects ; metabolism ; Gene Expression Regulation ; drug effects ; Glucose ; pharmacology ; Intercellular Adhesion Molecule-1 ; metabolism ; Intracellular Space ; drug effects ; metabolism ; Male ; Peritoneal Cavity ; cytology ; Peritoneal Dialysis ; Rats ; Rats, Sprague-Dawley

OBJECTIVETo develop a gene chip for rapid detection of the "a" determinant hotpoint mutation of hepatitis B virus (HBV).

METHODSPrimers were designed in the HBV conservative region, and probes for detecting 126A, 126S, 144A, 145R, 145E, 144A+145R, and 144A+145E mutants were developed for that gene chip. PCR amplification and gene chip technology were optimized. The performance of the gene chip was evaluated by detecting the reference plasmids. Forty five samples of serum obtained from patients with chronic hepatitis B were used to compare the sensitivity of the gene chip and the direct sequencing of PCR products.

RESULTSThe oligonucleotide microarray was specific for mutant and native plasmids. The sensitivity of the gene chip was 5 x 10(3)copies/micro l with a high reproducibility. The gene chip could detect minor variants when they were more than 10% among the HBV strains. The positive rates of 126A, 126S-1, 126S-2 detected in the 45 specimens by the gene chip (46.67%, 35.56% and 24.44%, respectively) were higher than those detected by direct sequencing of PCR products (9.00%, 4.44% and 2.22%; P=0.000, P=0.000 and P=0.002, respectively). The sequencing of cloned PCR products demonstrated that the gene chip was specific for the "a" determinant hotpoint mutation detection.

CONCLUSIONHBV "a" determinant hotpoint mutations can be detected by oligonucleotide microarray with high sensitivity and specificity, providing a method for large scale screening of the mutants.

Hepatitis B ; blood ; diagnosis ; Hepatitis B virus ; genetics ; Humans ; Oligonucleotide Array Sequence Analysis ; methods ; Point Mutation

OBJECTIVETo investigate effect of tramadol on c-fos expression in spinal cord dorsal horn and serum IL-6 levels induced by plantar incision in rats.

METHODSThe Brennan pain model was induced by incision on the planter surface of left hind paw in rats. Forty-eight rats were randomly divided into six groups: Sham group (Group C), control group (Group I,pretreatment with saline 5 ml), three tramadol pretreatment groups (Group T1, T10 and T20,pretreated with 1 mg/kg, 10 mg/kg and 20 mg/kg tramadol, respectively) and one tramadol treatment group (Group PT10, treated with tramadol 10 mg/kg immediately after operation). Pain behavior was assessed by withdrawal threshold to von Frey filament stimulation intensity, response latency of the hind paw to radiant thermal and a cumulative pain score 2 h after incision. Fos-positive neurons in spinal cord were identified by the immunohistochemical technique. Serum IL-6 levels were measured by enzyme-linked immunosorbent assay (ELISA).

RESULTSWithdrawIal threshold to von Frey filament stimulation intensity and response latency of the hind paw to radiant thermal in Group I were significantly lower than those in Group C (P<0.01). Cumulative pain score in Group I was significantly higher than that in Group C (P<0.01). In Groups of T10 and T20, withdrawal threshold to von Frey filament stimulation intensity and response latency of the hind paw to radiant thermal were significantly higher than those in Group I (P<0.01), cumulative pain score was significantly lower than that in Group I in a dose-dependent manner (P<0.01), and were also those in Group PT10. The greatest density of Fos-positive neurons was located in lamine I-II in Group I. Serum IL-6 levels were significantly elevated in Group I. Pretreatment with tramadol showed a dose-depended inhibitory effect on c-fos expression and serum IL-6 production,but not in Group T1. Administration of tramadol postoperatively also suppressed the c-fos expression and serum IL-6 production as showed in PT10 but were weaker than those in Group T10.

CONCLUSIONPretreatment with tramadol can produce dose-dependent inhibitory effect on c-fos expression in spinal cord dorsal horn and then suppress the inflammatory response to the trauma.

Analgesics, Opioid ; pharmacology ; therapeutic use ; Animals ; Interleukin-6 ; blood ; Male ; Pain Threshold ; drug effects ; Pain, Postoperative ; drug therapy ; metabolism ; Posterior Horn Cells ; drug effects ; metabolism ; Proto-Oncogene Proteins c-fos ; metabolism ; Random Allocation ; Rats ; Rats, Sprague-Dawley ; Tramadol ; pharmacology ; therapeutic use